摘要
目的研究利培酮薄膜衣片(抗精神分裂症药)在健康志愿者的药代动力学和生物等效性。方法23名健康男性志愿者随机交叉、单剂量口服受试制剂(进口)和参比制剂(国产)2mg后,用HPLC-MS/MS测定血浆中利培酮及9-羟基利培酮浓度,计算主要药代动力学参数,评价2种制剂的生物等效性。结果受试制剂和参比制剂的主要药代动力学参数,利培酮:AUC0～t分别为(94.76±82.93)和(103.05±117.71)ng.h.mL-1;AUC0～1分别为(96.72±84.52)和(105.19±119.36)ng.h.mL-1;Cmax分别为(15.91±5.63)和(16.21±11.56)ng·mL-1;tmax分别为(1.14±0.73)和(1.15±0.54)h;t1/2分别为(7.32±5.94)和(7.44±6.50)h,受试制剂的相对生物利用度为(106.68±40.21)%。9-羟基利培酮:AUC0～96h分别为(268.56±85.20)和(279.64±117.86)ng.h.mL-1;AUC0～∞分别为(282.74±87.46)和(294.28±120.32)ng.h.mL-1;Cmax分别为(10.84±4.69)和(11.11±4.80)ng·mL-1;tmax分别为(3.35±2.32)和(4.48±2.76)h;t1/2分别为(23.18±3.26)和(23.12±4.31)h,受试制剂的相对生物利用度为(101.37±27.23)%。结论2种制剂具有生物等效性。
Objective To study the pharmacokinetics and bioequivalence of risperidone filmcoated tablets in healthy volunteers. Methods A single administration of 2 mg risperidone of test and reference formulation was given to 23 healthy male volunteers according to an open, randomized, cross - over design. The concentration of risperidone and 9 - hydrorisperidone were determined by HPLC - MS/MS. The main pharmacokinetics were calculated and bioequivalence of two formulations were evaluated. Results The main pharmacokinetic parameters of test and reference formulation were as follows, risperidone： AUC0-t were（94.76±82.93 ） and（ 103.05±117.71 ）ng.h.mL^-1, AUC0-1 were （ 96.72±84.52） and （ 105.19 ±119.36） ng.h.mL^-1, Cmax were （ 15.91±5.63 ） and （ 16.21±11.56） ng.h.mL^-1 tmax were （1.14±0.73） and（1.15±0.54）h, h,t1/2 were （7.32±5.94） and （7.44±6.50 ） h, respectively. The relative bioavailability of risperidone was （ 106.68±40.21 ） % ; 9 - hydrorisperidone： AUC 0-96h were （268.56±85.20） and（279.64± 117.86）ng.h.mL^-1, AUC0_＊＊were（282.74±7.46）and（294.28±120.32）ng.h.mL^-1, Cm= were （10.84±4.69） and（11. 11±4.80）ng.h.mL^-1 tmax were （3.35±2.32） and（4.48±2.76）h, t1/2 were （23.18±3.26） and（23.12±4.31）h, respectively. The relative bioavailability of 9 - hydrorisperidone was （ 101.37±27.23 ） %. Conclusion The two formulations were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2009年第4期312-315,共4页
The Chinese Journal of Clinical Pharmacology
